Anti-estrogens have many purposes for the chemically enhanced athlete. Many of the drier “contest prep” androgens that bodybuilders use gain much of their affect due to antagonizing estrogen at both the receptor site and inhibiting its creation all together. For those that wish to not use anabolics then anti-estrogens are much desired because they can help you achieve a better hormonal alignment without actually having to ingest hormones. Anti-estrogens can:
- Prevent (or reverse) gyno
- Reduce estrogen related bloat
- Ensure a cycle with aromatizing androgens is drier/leaner
- Increase testosterone levels – very beneficial during PCT
- Aid in fat loss (estrogen is a lipogenic hormone)
Aromatase is the enzyme that converts male hormones to female estrogens. It is the primary way men create estrogen and failure to control this on cycles of aromatizing androgens like M14AD may produce very unsightly side effects. The most commonly used OTC anti-estrogens work through inhibiting this enzyme, and they will be covered below.
ATD is a supplement that gained huge exposure in numerous OTC PCT products over the past several years. It is a suicidal inhibitor of the aromatase enzyme, meaning that once the drug has been discontinued enzyme levels slowly return to baseline. Suicidal inhibitors are often preferred because there is no “rebound” in estrogens after coming off.
Scientific data on ATD shows it to be an effective anti estrogen and also would lead you to believe it produces immense increases in testosterone, however other data shows it produces a steroidal metabolite known as 1,4,6 Testosterone. The production of this weak androgen (about ⅓ the potency of testosterone) causes false readings on testosterone serum tests.ATD has huge amounts of anecdotal feedback claiming it markedly reduces sex drive, but it was largely speculated that this was due to a substantial decrease in estrogen (low or high estrogen in males will reduce libido). Scientific literature has pointed us in another direction and shown that ATD is actually anti-androgenic (the complete opposite of what we would want).
The claims that this is great in PCT are nil when the data has been observed. It will reduce estrogen, but also occupy the androgen receptor and not allow testosterone to bind. The 1,4,6 testosterone metabolite would also theoretically produce HPTA suppression if the dose is significant.
ATD Pros:
- Reduces Estrogen
- Suicidal Inhibitor
- Possibly HPTA Suppressive
- Anti-Androgenic
- May Reduce Sex Drive
Common Products:
- Inhibit-E
- Novedex XT
Formestane is another suicidal inhibitor of the aromatase enzyme. It was originally studied as a pharmaceutical injection treatment for breast cancer but was pulled off the market in favor of other anti-estrogenic drugs. Formestane has been shown to reduce estrogen content within the body by 50%, so while not being as potent as some pharmaceuticals it does provide a nice reduction in levels.
Formestane will convert to the substance 4-hydroxytestosterone within the body, and this may make it hinder recovery if used during PCT. Formestane and 4-hydroxytestosterone can inhibit the enzyme 5-alpha reductase, which is responsible for creating DHT. This also makes formestane a less desired approach to combat gyno because DHT is our bodies natural defense against estrogen. Studies even show that DHT therapy alone can reverse gyno in men, so it isnt exactly something suitable if reducing it might cost you a pair of moobs. Reduction of 5-alpha reductase is favorable for those prone to male pattern baldness, so those ingesting aromatizing androgens may have a safer bet using formestane to mildly reduce androgenic hormones and also estrogen if hair loss, but not gyno, is a concern.
Formestane has very poor oral bioavailability so a transdermal preparation is often the preferred mode for ingesting this substance. If oral products are to be used doses should be 150+mg per day.
Formestane Pros:
- Reduces Estrogen
- Better for those prone to hair loss
- Suicidal Inhibitor Best Used Topically
- Possibly HPTA Suppressive
- Not as Effective for Gyno
Common Products
- CEL Formestane (Topical)
- Primordial Performance Formestane (Oral)
Androsta-3,5-diene-7,17-dione
(Erase)
This is the newest anti-estrogenic compound on the market. It is a suicidal inhibitor like the others above but has a few distinct alterations. First, this compound is unable to convert to a steroidal metabolite. This means that it is very favorable during PCT because HPTA suppression is impossible. The 7-oxo that this compound has also makes it good at reducing the catabolic hormone cortisol, which spikes after coming off your cycle.
Studies on the affinity for the aromatase enzyme show that this compound is actually more potent than the pharmaceutical compound Aromasin. The difference in bioavailability between the two is in favor of Aromasin, so that means that this compound would need to be ingested at slightly greater dosages (50-75mg vs 25mg).
Androst-3,5-dien-7,17-dione Pros:
- Potently Reduces Estrogen
- Suicidal Inhibitor
- Reduces Cortisol
- Strong In-Vitro Data
- Lacking In-Vivo Data
- PES Erase
- Erase Pro
Aromatizing Prohormones
Anti Estrogens should be considered on any of the following compounds to reduce the likelihood of side effects:
- Methyl 1,4-AD (M14AD)
- Ment Dione
- M-LMG
- Boladrol
Anti-estrogens may not be needed on cycles containing prohormones that do not convert to estrogen, but there has been reports of hormones causing gyno regardless of estrogen conversion. This likely happens from the bodies response to increased androgen levels, which then causes adrenal hormones to convert more readily into estrogens. This can also be combated by using one of the above anti-estrogens, and should typically be your first resort if pharmaceutical preparations are not within reach.
Disclaimer
We are not doctors, therefore before starting any supplement or training regiment you should consult with your doctor. The information being provided is simply personal opinion.


